Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue

Price David A.,Eng Heather,Farley Kathleen A.,Goetz Gilles H.,Huang Yong, Jiao Zhaodong,Kalgutkar Amit S.,Kablaoui Natasha M.,Khunte Bhagyashree,Liras Spiros,Limberakis Chris,Mathiowetz Alan M.,Ruggeri Roger B.,Quan Jun-Min,Yang Zhen

Organic & Biomolecular Chemistry（2017）

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摘要

The synthesis and in vivo pharmacokinetic profile of an analogue of cyclosporine is disclosed. An acyclic congener was also profiled in in vitro assays to compare cell permeability. The compounds possess similar calculated and measured molecular descriptors however have different behaviors in an RRCK assay to assess cell permeability.

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